A Method for the Racemization of 2-Methylpyrrolidine: A Histamine H3 Receptor Pharmacophore
详细信息 查看全文
- 作者：Swapnil G. Yerande ; Ragini S. Yerande ; Prashant P. Thakare ; Deepak M. Shendage ; Sharad Galave ; Ashok Kumar Gangopadhyay
- 刊名：Organic Process Research & Development
- 出版年：2014
- 出版时间：May 16, 2014
- 年：2014
- 卷：18
- 期：5
- 页码：652-655
- 全文大小：199K
- 年卷期：v.18,no.5(May 16, 2014)
- ISSN：1520-586X
文摘
This paper describes a method for the racemization of unwanted (S)-1 isomer arising from the resolution of (卤)-1. The process of racemization involves thiyl radical-mediated reversible hydrogen abstraction at the chiral center, in the presence of AIBN in water. The racemized isomer was subsequently resolved by l-(+)-tartaric acid to get (R)-1, a histamine H3 receptor pharmacophore. We foresee that such an approach of racemization will be industrially useful for recycling waste (S)-1 enantiomer.